Chemical genetics of Plasmodium falciparum

Nature

Volumn 465, Issue 7296, 2010, Pages 311-315

  Guiguemde, W Armand ^a   Shelat, Anang A ^a   Bouck, David ^a   Duffy, Sandra ^b   Crowther, Gregory J ^c   Davis, Paul H ^d   Smithson, David C ^a   Connelly, Michele ^a   Clark, Julie ^a   Zhu, Fangyi ^a   Jiménez Díaz, María B ^e   Martinez, María S ^e   Wilson, Emily B ^f   Tripathi, Abhai K ^g   Gut, Jiri ^f   Sharlow, Elizabeth R ^h   Bathurst, Ian ⁱ   Mazouni, Farah El ^j   Fowble, Joseph W ^c   Forquer, Isaac ^k   McGinley, Paula L ^l   Castro, Steve ^l   Angulo Barturen, Iñigo ^e   Ferrer, Santiago ^e   Rosenthal, Philip J ^f   Derisi, Joseph L ^f   Sullivan Jr , David J ^g   Lazo, John S ^h   Roos, David S ^d   Riscoe, Michael K ^k   Phillips, Margaret A ^j   Rathod, Pradipsinh K ^c   Van Voorhis, Wesley C ^c   Avery, Vicky M ^b   Guy, R Kiplin ^a   more..

^a ST JUDE CHILDREN S RESEARCH HOSPITAL   (United States)

^b GRIFFITH UNIVERSITY   (Australia)

^c UNIVERSITY OF WASHINGTON   (United States)

^d UNIVERSITY OF PENNSYLVANIA   (United States)

^e GLAXOSMITHKLINE   (Spain)

^f UNIVERSITY OF CALIFORNIA   (United States)

^g JOHNS HOPKINS BLOOMBERG SCHOOL OF PUBLIC HEALTH   (United States)

^h UNIVERSITY OF PITTSBURGH SCHOOL OF MEDICINE   (United States)

ⁱ Medicines for Malaria Venture   (Switzerland)

^j UNIVERSITY OF TEXAS SOUTHWESTERN MEDICAL CENTER   (United States)

^k PORTLAND VA MEDICAL CENTER   (United States)

^l RUTGERS UNIVERSITY   (United States)

more..

Author keywords

[No Author keywords available]

Indexed keywords

AMINOQUINOLINE DERIVATIVE; AMODIAQUINE; ARTEMISININ; ATOVAQUONE; BENZIMIDAZOLE; BENZOFURAN DERIVATIVE; CARBAZOLE DERIVATIVE; CHLOROQUINE; CYCLOGUANIL; DIHYDROPYRIDINE; DIHYDROPYRIDINE DERIVATIVE; MEFLOQUINE; MICROORGANISM PROTEIN; NEW DRUG; QUINAZOLINE; QUININE; QUINOLONE DERIVATIVE;

ANTIMALARIAL AGENT; BIOACTIVITY; BIOCHEMISTRY; DISEASE CONTROL; DRUG DEVELOPMENT; DRUG RESISTANCE; GENETICS; MALARIA; PHENOTYPE; PROTEIN; PROTOZOAN; VACCINE;

ANTIMALARIAL ACTIVITY; ANTIMALARIAL DRUG RESISTANCE; ARTICLE; ASSAY; BIOLOGICAL ACTIVITY; CELL LINE; CHEMICAL GENETICS; CHEMICAL STRUCTURE; CHEMISTRY; CONTROLLED STUDY; DNA FINGERPRINTING; DRUG POTENCY; DRUG TARGETING; EMBRYO; GENE IDENTIFICATION; GENE LIBRARY; GENETIC SIMILARITY; HUMAN; HUMAN CELL; IN VITRO STUDY; MAMMAL CELL; NONHUMAN; PHENOTYPE; PLASMODIUM FALCIPARUM; PRIORITY JOURNAL; PROTEIN BINDING; TOXOPLASMA GONDII;

ANIMALS; ANTIMALARIALS; CELL LINE; DRUG DISCOVERY; DRUG EVALUATION, PRECLINICAL; DRUG RESISTANCE; DRUG THERAPY, COMBINATION; ERYTHROCYTES; HUMANS; MALARIA, FALCIPARUM; MICE; PHENOTYPE; PHYLOGENY; PLASMODIUM FALCIPARUM; REPRODUCIBILITY OF RESULTS; SMALL MOLECULE LIBRARIES;

MAMMALIA; MURINAE; PLASMODIUM FALCIPARUM; PROTOZOA; TOXOPLASMA GONDII;

EID: 77952718950     PISSN: 00280836     EISSN: 14764687     Source Type: Journal    
DOI: 10.1038/nature09099     Document Type: Article

References (27)

1. Wongsrichanalai, C. & Meshnick, S. R. Declining artesunate-mefloquine efficacy against falciparum malaria on the Cambodia-Thailand border. Emerg. Infect. Dis. 14, 716-719 (2008). (Pubitemid 351838633)
2. Dondorp, A. M. et al. Artemisinin resistance in Plasmodium falciparum malaria. N. Engl. J. Med. 361, 455-467 (2009).
3. Ridley, R. G. Medical need, scientific opportunity and the drive for antimalarial drugs. Nature 415, 686-693 (2002).
4. Kissinger, J. C. et al. The Plasmodium genome database. Nature 419, 490-492 (2002).
5. Baniecki, M. L., Wirth, D. F. & Clardy, J. High-throughput Plasmodium falciparum growth assay for malaria drug discovery. Antimicrob. Agents Chemother. 51, 716-723 (2007). (Pubitemid 46185294)
6. Plouffe, D. et al. In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen. Proc. Natl Acad. Sci. USA 105, 9059-9064 (2008).
7. Weisman, J. L. et al. Searching for new antimalarial therapeutics amongst known drugs. Chem. Biol. Drug Des. 67, 409-416 (2006).
8. Wells, T. N., Alonso, P. L. & Gutteridge, W. E. New medicines to improve control and contribute to the eradication of malaria. Nature Rev. Drug Discov. 8, 879-891 (2009).
9. Munos, B. Can open-source R&D reinvigorate drug research? Nature Rev. Drug Discov. 5, 723-729 (2006). (Pubitemid 44323699)
10. Shelat, A. A. & Guy, R. K. Scaffold composition and biological relevance of screening libraries. Nature Chem. Biol. 3, 442-446 (2007).
11. Shelat, A. A. & Guy, R. K. The interdependence between screening methods and screening libraries. Curr. Opin. Chem. Biol. 11, 244-251 (2007).
12. Smilkstein, M. et al. Simple and inexpensive fluorescence-based technique for high-throughput antimalarial drug screening. Antimicrob. Agents Chemother. 48, 1803-1806 (2004). (Pubitemid 38544392)
13. Cibulskis, R. E. et al. Estimating trends in the burden of malaria at country level. Am. J. Trop. Med. Hyg. 77 (suppl. 6), 133-135 (2007).
14. Gujjar, R. et al. Identification of a metabolically stable triazolopyrimidine-based dihydroorotate dehydrogenase inhibitor with antimalarial activity in mice. J. Med. Chem. 52, 1864-1872 (2009).
15. Patel, V. et al. Identification and characterization of small molecule inhibitors of Plasmodium falciparum dihydroorotate dehydrogenase. J. Biol. Chem. 283, 35078-35085 (2008).
16. Weissbuch, I. & Leiserowitz, L. Interplay between malaria, crystalline hemozoin formation, and antimalarial drug action and design. Chem. Rev. 108, 4899-4914 (2008).
17. Pisciotta, J. M. et al. The role of neutral lipid nanospheres in Plasmodium falciparum haem crystallization. Biochem. J. 402, 197-204 (2007). (Pubitemid 46254920)
18. Sijwali, P. S. & Rosenthal, P. J. Gene disruption confirms a critical role for the cysteine protease falcipain-2 in hemoglobin hydrolysis by Plasmodium falciparum. Proc. Natl Acad. Sci. USA 101, 4384-4389 (2004).
19. Sijwali, P. S., Koo, J., Singh, N. & Rosenthal, P. J. Gene disruptions demonstrate independent roles for the four falcipain cysteine proteases of Plasmodium falciparum. Mol. Biochem. Parasitol. 150, 96-106 (2006). (Pubitemid 44332580)
20. Crowther, G. J. et al. Buffer optimization ofthermal meltassaysofPlasmodiumproteins for detection of small-molecule ligands. J. Biomol. Screen. 14, 700-707 (2009).
21. Witola, W. H. et al. Disruption of the Plasmodium falciparum PfPMT gene results in a complete loss of phosphatidylcholine biosynthesis via the serine-decarboxylase-phosphoethanolamine-methyltransferase pathway and severe growth and survival defects. J. Biol. Chem. 283, 27636-27643 (2008).
22. Krnajski, Z. et al. Thioredoxin reductase is essential for the survival of Plasmodium falciparum erythrocytic stages. J. Biol. Chem. 277, 25970-25975 (2002). (Pubitemid 34967078)
23. McFadden, G. I. & Roos, D. S. Apicomplexan plastids as drug targets. Trends Microbiol. 7, 328-333 (1999).
24. Reynolds, M. G. & Roos, D. S. A biochemical and genetic model for parasite resistance to antifolates. Toxoplasma gondii provides insights into pyrimethamine and cycloguanil resistance in Plasmodium falciparum. J. Biol. Chem. 273, 3461-3469 (1998).
25. Lipinski, C. A., Lombardo, F., Dominy, B. W. & Feeney, P. J. Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings. Adv. Drug Deliv. Rev. 46, 3-26 (2001). (Pubitemid 33653411)
26. Shenai, B. R. et al. Structure-activity relationships for inhibition of cysteine protease activity and development of Plasmodium falciparum by peptidyl vinyl sulfones. Antimicrob. Agents Chemother. 47, 154-160 (2003).
27. Ritz, C. & Streibig, J. C. Bioassay analysis using R. J. Stat. Softw. 12, 22 (2005).